LitoXetine is a novel selective serotonin reuptake inhibitor (SSRI) with a unique chemical structure. It has been shown to exhibit potent antidepressant activity in preclinical studies, and it is currently undergoing clinical trials for the treatment of major depressive disorder (MDD). The specific synthesis process for LitoXetine has not been publicly disclosed, likely due to its proprietary nature. LitoXetine is a relatively new compound, and research on its effects, importance, and why it is studied is ongoing. LitoXetine is being studied because of its potential to offer a novel treatment option for MDD with a potentially improved side effect profile compared to existing SSRIs. The unique chemical structure of LitoXetine may provide advantages in terms of pharmacokinetic properties, such as improved absorption, distribution, metabolism, and excretion. LitoXetine is also being investigated for its potential to be effective in treating other psychiatric conditions, such as anxiety disorders.'
litoxetine: a serotonin uptake inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 65650 |
| CHEMBL ID | 471036 |
| SCHEMBL ID | 119884 |
| MeSH ID | M0159839 |
| Synonym |
|---|
| 4-(naphthalen-2-ylmethoxy)piperidine |
| CHEMBL471036 , |
| litoxetine |
| bdbm50278564 |
| 9980st005g , |
| litoxetina |
| litoxetinum [inn-latin] |
| unii-9980st005g |
| 86811-09-8 |
| 4-(2-naphthylmethoxy)piperidine |
| litoxetina [inn-spanish] |
| litoxetinum |
| litoxetine [inn] |
| SCHEMBL119884 |
| DTXSID30235828 |
| DB15038 |
| Q6648700 |
| sl 81-0385; sl 810385 |
Litoxetine is a selective serotonin reuptake inhibitor with antidepressant activity in animal models and in depressed patients.
| Excerpt | Reference | Relevance |
|---|---|---|
| "1. Litoxetine is a selective serotonin reuptake inhibitor with antidepressant activity in animal models and in depressed patients. " | ( EEG profile of litoxetine after single and repeated administration in healthy volunteers. Bianchetti, G; Court, LA; Dubruc, C; Morselli, PL; Patat, A; Rosenzweig, P; Thébault, JJ; Trocherie, S, 1994) | 1.26 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Litoxetine has moderate affinity for cerebral 5HT3 receptors (Ki = 85 nM), while fluoxetine, similar to other 5HT uptake inhibitors, has only negligible affinity for this receptor (Ki = 6.5 microM)." | ( Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties. Angel, I; Garreau, M; Langer, SZ; Prouteau, M; Schoemaker, H, 1993) | 2.45 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " These effects occurred with litoxetine blood concentrations ranging from 3 to 7 ng ml-1 with the 10 mg dosage and from 8 to 18 ng ml-1 with the 25 mg dosage." | ( EEG profile of litoxetine after single and repeated administration in healthy volunteers. Bianchetti, G; Court, LA; Dubruc, C; Morselli, PL; Patat, A; Rosenzweig, P; Thébault, JJ; Trocherie, S, 1994) | 0.93 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cannabinoid receptor 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.4000 | 0.0002 | 0.6609 | 10.0000 | AID445757 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 (µMol) | 3.9500 | 0.0008 | 1.5416 | 20.0000 | AID416799; AID445757 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 (µMol) | 0.0060 | 0.0001 | 0.8645 | 8.7096 | AID416798; AID445756 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 (µMol) | 4.0000 | 0.0007 | 1.8419 | 46.0000 | AID416800; AID445758 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID416800 | Inhibition of radiolabeled dopamine reuptake at human DAT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. |
| AID445758 | Inhibition of dopamine reuptake at human dopamine transporter expressed in HEK293 cells after 5 mins by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
| AID416799 | Inhibition of radiolabeled noradrenaline reuptake at human NET expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. |
| AID445756 | Inhibition of serotonin reuptake at human serotonin transporter expressed in HEK293 cells after 5 mins by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
| AID445755 | Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
| AID445757 | Inhibition of noradrenaline reuptake at human noradrenaline transporter expressed in HEK293 cells after 15 mins by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
| AID416798 | Inhibition of radiolabeled serotonin reuptake at human SERT expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8 | Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (11.11) | 18.7374 |
| 1990's | 5 (55.56) | 18.2507 |
| 2000's | 2 (22.22) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 1 (11.11) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.60) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (33.33%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||